2206736-04-9
2206736-04-9 structure
- Name: MRTX1257
- Chemical Name: MRTX-1257
- CAS Number: 2206736-04-9
- Molecular Formula: C33H39N7O2
- Molecular Weight: 565.71
- Catalog: Signaling Pathways GPCR/G Protein Ras
- Create Date: 2019-07-04 19:38:54
- Modify Date: 2024-01-12 09:51:26
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MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1].
| Name | MRTX-1257 |
|---|
| Description | MRTX-1257 is a selective, irreversible, covalent and oral active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells[1]. |
|---|---|
| Related Catalog | |
| Target |
IC50: 900 pM (KRAS dependent ERK phosphorylation in H358 cells)[1]. |
| In Vivo | MRTX-1257 (1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg, orally, daily for 30 days) shows rapid tumor growth inhibition at all dose groups in MIA PaCa-2 G12C Xenograft model in mice[1]. MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups[1]. MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained >70 days after cessation of treatment[1]. Animal Model: MIA PaCa-2 G12C Xenograft Model (mouse)[1]. Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg. Administration: Orally daily for 30 days. Result: Showed rapid tumor growth inhibition at all dose groups. Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups. 100 mg/kg daily led to complete responses that are maintained >70 days after cessation of treatment. |
| References |
| Molecular Formula | C33H39N7O2 |
|---|---|
| Molecular Weight | 565.71 |